PL EN


Preferencje help
Widoczny [Schowaj] Abstrakt
Liczba wyników
1999 | 46 | 3 |

Tytuł artykułu

Modelling of insulin receptor tyrosine kinase in its active form: a case study for validation of theoretical methods

Warianty tytułu

Języki publikacji

EN

Abstrakty

EN
An active form of an insulin receptor tyrosine kinase (IRK) catalytic core was modelled based on its experimentally known inactive form and the active form of a serine/threonine kinase, protein kinase A (PKA). This theoretical model was compared with the crystallographic structure of the active form of IRK reported later. The structures are very similar, which shows that all the most important features and interactions have been taken into account in the modelling procedure. The elaborated procedure can be applied to other tyrosine kinases. This would allow designing of a wide class of tyrosine kinase inhibitors, very important potential anti-cancer and/or anti-viral drugs.

Wydawca

-

Rocznik

Tom

46

Numer

3

Opis fizyczny

p.601-607,fig.

Twórcy

autor
  • Warsaw University, S.Zwirki i F.Wigury 93, 02-089 Warsaw, Poland
autor

Bibliografia

  • 1. Hunter, T. (1991) Protein kinase classifica­tion. Methods EnzymoL 200, 3-37.
  • 2. Cox, S., Radzio-Andzelm, E. & Taylor, S.S. (1994) Domain movements in protein kinases. Curr. Opiru Struct. Biol 4, 893-901.
  • 3. White, M.F. & Kahn, C.R. (1994) The insulin signaling system. J. Biol. Chem. 269, 1-4.
  • 4. Ebina, Y., Ellis, L., Jarnagin, K., Edery, M., Graf, L., Clauser, E,, Ou, J.H., Masiarz, F., Kan, Y.W., Goldfine, I.D., Roth, R.A. & Rutter, W.J. (1985) The human insulin recep­tor cDNA: The structural basis for hormone- activated transmembrane signalling. Cell 40, 747-758.
  • 5. Ullrich, A., Bell, J.R., Chen, E.Y., Herrera, R., Petruzzelli, L.M., Dull, TJ., Gray, A., Coussens, L., Liao, Y.C., Tsubokawa, M., Ma­son, A., Seeburg, P.H., Grunfeld, C., Rosen, O.M. & Ramachandran, J. (1985) Human insu­lin receptor and its relationship to the tyrosine kinase family of oncogenes. Nature 313, 756-761.
  • 6. Wei, L.. Hubbard, S.R., Hendrickson, W.A. & Ellis, L. (1995) Expression, characterization, and crystallization of the catalytic core of the human insulin receptor protein-tyrosine kinase domain. J. Biol Chem. 270, 8122-8130.
  • 7. Rosen, O.M., Herrera, R., Olowe, Y., Petru­zzelli, L.M. & Cobb, M.H. (1983) Phospho­rylation activates the insulin receptor tyrosine protein kinase. Proc. Natl Acad. Sci. U.S.A. 80, 3237-3240.
  • 8. Ellis, L., Clauser, E., Morgan, D.O., Edery, M., Roth, R.A. & Rutter, W.J. (1986) Replacement of insulin receptor tyrosine residues 1162 and 1163 compromises insulin-stimulated kinase activity and uptake of 2-deoxyglucose. Cell 45, 721-732.
  • 9. Hubbard, S.R., Wei, L., Ellis, L. &. Hen­drickson, W.A. (1994) Crystal structure of the tyrosine kinase domain of the human insulin receptor. Nature 372, 746-754.
  • 10. Ginalski, K., Lesyng, B., Sowadski, J. & Wojciechowski, M. (1997) Modelling of active forms of protein kinases: p38 — A case study. Acta Biochim. Poloru 44, 557-564.
  • 11. Miller, M., Zbar, B., Ginalski, K. & Lesyng, B. (1998) Structural basis of oncogenesis caused by point mutations in the kinase domain of the MET proto-oncogene. Cell Mol Biol Lett 3, 273-274.
  • 12. Hubbard, S.R. (1997) Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP ana­log. EMBOJ. IB, 5572-5581.
  • 13. Zheng, J., Trafny, E.A., Knighton, D.R., Xuong, N.-H., Taylor, S.S., Ten Eyck, L.F. & Sowadski, J.M. (1993) 2.2 A refined crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MnATP and peptide inhibitor. Acta Crystallog. D 49, 362-365.
  • 14. INSIGHT II User Guide, Version 95.0 (1995) Biosym Technologies, San Diego.
  • 15. Zhou, S., Carraway III, K.L., Eck, M.J., Harri­son, S.C., Feldman, R.A., Mohammadi, M., Schlessinger, J., Hubbard, S.R., Smith, D.P., Eng, C., Lorenzo, M.J., Ponder, B.A.J., Mayer, B.J. & Cantley, L.C. (1995) Catalytic specific­ity of protein-tyrosine kinases is critical for se­lective signalling. Nature 373, 536- 539.
  • 16. DISCOVER User Guide, Version 95.0 (1995) Biosym Technologies, San Diego.
  • 17. Weiner, S.J., KoUman, P.A., Case, D.A., Singh, U.C., Ghio, C., Alagona, G., Profeta, S., Jr. & Weiner, P. (1984) A new force field for molecular mechanical simulation of nucleic ac­ids and proteins. J. Am. Chem. Soc. 106, 765-784.
  • 18. Kabsch, W. & Sander, C. (1983) Dictionary of protein secondary structure: Pattern recogni­tion of hydrogen-bonded and geometrical fea­tures. Biopolymers 22, 2577-2637.

Typ dokumentu

Bibliografia

Identyfikatory

Identyfikator YADDA

bwmeta1.element.agro-article-76c3b8a4-dd58-463c-ba7b-b844952ec803
JavaScript jest wyłączony w Twojej przeglądarce internetowej. Włącz go, a następnie odśwież stronę, aby móc w pełni z niej korzystać.